Disposition of Intravenous Pirmenol

Abstract
Twelve patients having frequent premature ventricular complexes (PVC) averaging more than 60/h received a single 150-mg i.v. dose of pirmenol. Plasma pirmenol concentration declined biexponentially following the infusion and was analyzed according to a 2-compartment open model. Following an erratic distribution phase, the terminal elimination half-life (t1/2) ranged from 4.2-16.9 h, with a geometric mean of 7.6 h. Total body clearance averaged 164 .+-. 58 ml/min, and the mean volume of distribution was 1.45 .+-. 0.38 l/kg. Renal clearance averaged 46.6 .+-. 21.2 ml/min, representing 30 .+-. 10% of total body clearance. Excretion of unchanged drug in the urine averaged 31.8 .+-. 8% of the dose. Renal clearance and elimination t1/2 were correlated (r = -0.61, P < 0.05). Eight of the 12 patients achieved > 95% suppression of PVC with a duration between 20 min and 23 h. These favorable pharmacokinetics indicate that pirmenol may be a useful addition to the therapy of ventricular arrhythmias.